Background: Curcumin is a polyphenolic natural compound with multiple targets that used
for the prophylaxis and treatment of some type of cancers like cervical and pancreatic cancers. Some
recent patent for curcumin for cancer has also been reviewed.
Objective: In this study, ten new curcumin derivatives were designed and synthesized and their cytostatic activity evaluated
against the Hela and Panc cell lines that some of them showed more activity than curcumin.
Method: In the present study, a series of mono-carbonyl derivatives of curcumin were designed and prepared. The details
of the synthesis and chemical characterization of the synthesized compounds are described. The cytostatic activities of the
designed compounds are assessed in two different tumor cell lines using MTT test.
Results: In vitro screening for human cervix carcinoma cell lines (Hela) and pancreatic cell lines (Panc-1) at 24 and 48
hour showed that all the analogs possessed good activity against these tumor cell lines and compounds 5a, 5c and 6 with
high potency can be used as a new lead compounds for the designing and finding new and potent cytostatic agents. Docking
studies indicated that compound 5c readily binds the active site of human glyoxalase I protein via two strong hydrogen
bonds engaging residues of Glu-99 and Lys-156.
Conclusion: Our results are useful in guiding a design of optimized ligands with improved pharmacokinetic properties
and increased of anti-cancer activity vs. the prototype curcumin compound.